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通过静电纺丝技术将含有苦味模型药物的乙基纤维素微粒掺入纳米纤维垫中——初步研究

Incorporation of Ethylcellulose Microparticles Containing a Model Drug with a Bitter Taste into Nanofibrous Mats by the Electrospinning Technique-Preliminary Studies.

作者信息

Olechno Katarzyna, Grilc Nina Katarina, Zupančič Špela, Winnicka Katarzyna

机构信息

Department of Pharmaceutical Technology, Medical University of Bialystok, Mickiewicza 2c, 15-222 Bialystok, Poland.

Department of Pharmaceutical Technology, University of Ljubljana, Aškerčeva c. 7, 1000 Ljubljana, Slovenia.

出版信息

Materials (Basel). 2022 Jul 31;15(15):5286. doi: 10.3390/ma15155286.

Abstract

Electrospinning is considered a simple and comprehensive technique to formulate ultrafine fibres by using an electric field. Polymeric nanofibers constitute promising materials in biomedical applications as drug delivery systems. For their preparation, both natural and synthetic polymers are utilised. Owing to the potential use of electrospun nanofibers as an orodispersible drug dosage form, ethylcellulose microparticles containing the antihistamine drug rupatadine fumarate, prepared by the spray drying technique to conceal the drug's bitter taste, were incorporated into nanofibers. The obtained nanofibrous mats were evaluated for morphology, mechanical strength, disintegration time, the drug solid state and acceptability in terms of taste masking efficiency. Preliminary studies showed that hypromellose used as a single polymer was not a suitable substance for the manufacturing of nanofibers. Therefore, in order to facilitate the obtention of homogeneous nonwovens, different grades of polyethylene oxide (2,000,000-2M-Da and 4,000,000-4M-Da) were added, which improved the quality of the prepared mats. Nanofibers of the most satisfactory quality were obtained from hypromellose (6.5% /) and PEO (2M, 0.5% /). SEM image analysis has shown that the nanofibers were homogeneous and smooth and possessed a fast disintegration time (below 30 s) and an adequate drug content with a simultaneous taste-masking effect (as indicated by the in vivo and in vitro methods). However, further studies are necessary to refine their mechanical characteristics.

摘要

静电纺丝被认为是一种利用电场制备超细纤维的简单而全面的技术。聚合物纳米纤维作为药物递送系统,在生物医学应用中构成了有前景的材料。对于它们的制备,天然和合成聚合物都被使用。由于静电纺纳米纤维有作为口腔崩解药物剂型的潜在用途,通过喷雾干燥技术制备的含有抗组胺药物富马酸卢帕他定的乙基纤维素微粒被掺入纳米纤维中,以掩盖药物的苦味。对获得的纳米纤维垫进行了形态、机械强度、崩解时间、药物固态以及掩味效率方面的可接受性评估。初步研究表明,用作单一聚合物的羟丙甲纤维素不是制造纳米纤维的合适物质。因此,为了便于获得均匀的无纺布,添加了不同等级的聚环氧乙烷(2,000,000 - 2M - Da和4,000,000 - 4M - Da),这提高了制备垫的质量。从羟丙甲纤维素(6.5% /)和聚环氧乙烷(2M,0.5% /)获得了质量最令人满意的纳米纤维。扫描电子显微镜图像分析表明,纳米纤维均匀且光滑,具有快速崩解时间(低于30秒)和足够的药物含量,同时具有掩味效果(体内和体外方法表明)。然而,需要进一步研究来优化它们的机械特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0ff3/9369697/69a08aa5d176/materials-15-05286-g001.jpg

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